Home > DNA/RNA Synthesis & > Temozolomide

Temozolomide

替莫唑胺,CCRG81045, NSC 362856

Temozolomide是一种DNA损伤诱导剂,烷化剂。

目录号
EY0671
EY0671
EY0671
EY0671
纯度
99.58%
99.58%
99.58%
99.58%
规格
5 mg
10 mg
50 mg
100 mg
原价
235
378
621
770
售价
235
378
621
770
库存
现货
现货
现货
现货
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  • 生物活性

    Temozolomide is an antitumor, antiangiogenic compound that has been shown to work by alkylating DNA, typically through addition of a methyl group to guanine in genomic DNA. The efficacy of this compound is dependent on its ability to methylate the DNA, thus triggering apoptosis; however, some cells are able to repair this damage via the enzymes O-6-methylguanine-DNA methyltransferase (MGMT). As a consequence, temozolomide is far more efficacious in tumor cells that have silenced this repair enzyme. Furthermore, temozolomide has been implicated in causing arrest at the G2/M cell cycle checkpoint, which might also play a role in its cytotoxicity. Displays antitumor activity against a board spectrum of tumors, including leukemias, lymphomas and solid tumors (IC50 = 5.0 μM for cytotoxicity against mouse TLX5 lymphoma cells). Induces autophagy in malignant glioma cells. Exhibits enhanced activity when used in combination with CHC.

  • 体外研究

  • 体内研究

    1% DMSO+30% polyethylene glycol+1% Tween 80

  • 激酶实验

  • 细胞实验

    0 μM -100 μM

  • 动物实验

    40 mg/kg 静脉注射给药

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Catapano CV, et al. Cancer Res. 1987, 47(18), 4884-4889.
    [2] Stevens, M.F., et al. 1984. J. Med. Chem. 27: 196-201.
    [3] Stevens, M.F., et al. 1984. J. Med. Chem. 27: 196-201.
    [3] Tentori, L., et al. 2002. Blood. 99: 2241-2244.
    [4] Kurzen, H., et al. 2003. Anticancer Drugs. 14: 515-522.
    [5] Günther, W., et al. 2003. Br. J. Cancer. 88: 463-469.
    [6] Beier, D., et al. 2008. Cancer Res. 68: 5706-5715.
    [7] Quinn, J.A., et al. 2009. J. Clin. Oncol. 27: 1262-1267.

    分子式
    C6H6N6O2    		 分子量
    194.15    		 CAS号
    85622-93-1    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    39 mg/mL    		 Water
    5 mg/mL    		 Ethanol
    <1 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00619112 Recurrent Central Nervous System Neoplasm Drug: temozolomide University of California, San Francisco|National Cancer Institute (NCI) Phase 2 2007-10-01 2013-10-29
    NCT01847235 Anaplastic Oligodendroglioma|Anaplastic Oligoastrocytoma Drug: Temozolomide Seoul National University Hospital Phase 2 2013-05-01 2016-04-22
    NCT00012116 Metastatic Cancer Drug: temozolomide Jonsson Comprehensive Cancer Center|National Cancer Institute (NCI)|Schering-Plough Phase 2 2000-10-01 2015-10-28
    NCT01114555 Neuroblastoma Drug: Bevacizumab, Irinotecan and Temozolomide Memorial Sloan Kettering Cancer Center|Genentech, Inc. Phase 2 2010-04-01 2016-05-09
    NCT02972320 Extensive Stage Small Cell Lung Cancer Drug: temozolomide Yunpeng Liu|China Medical University, China Phase 2 2016-06-01 2016-11-22
    NCT00629187 Central Nervous System Neoplasms|Neoplasm Metastasis Drug: Temozolomide Tufts Medical Center Phase 1 2004-04-01 2012-04-26
    NCT00612339 Glioblastoma|Gliosarcoma Drug: Avastin and Temozolomide Duke University|Genentech, Inc.|Schering-Plough Phase 2 2007-08-01 2013-05-20
    NCT00400816 Central Nervous System Tumors|Brain Tumor Drug: temozolomide The Cleveland Clinic|National Cancer Institute (NCI) Phase 2 2005-08-01 2016-08-06
    NCT00392171 Glioma|Astrocytoma|Oligodendroglioma|Glioblastoma Drug: Temozolomide Schering-Plough Phase 2 2006-06-01 2010-06-03
    NCT01067066 Melanoma Drug: TPI 287|Drug: Temodar (Temozolomide) M.D. Anderson Cancer Center|Cortice Biosciences, Inc. Phase 1|Phase 2 2010-02-01 2016-07-07
    NCT02340156 GLIOBLASTOMA Genetic: SGT-53|Drug: Temozolomide SynerGene Therapeutics, Inc. Phase 2 2014-12-01 2016-11-23
    NCT02113007 Primary Central Nervous System Lymphoma Drug: Rituximab plus Temozolomide SCRI Development Innovations, LLC|Genentech, Inc. Phase 2 2014-07-01 2016-12-14
    NCT00740636 Lung Cancer Drug: Temozolomide|Drug: Temozolomide Memorial Sloan Kettering Cancer Center|Schering-Plough Phase 2 2008-08-01 2016-07-01
    NCT00925132 Metastatic Melanoma Drug: Temozolomide, Decitabine, Panobinostat University of Iowa|Holden Comprehensive Cancer Center|Novartis Pharmaceuticals Phase 1|Phase 2 2009-12-01 2017-01-04
    NCT00313729 CNS Tumor, Adult Drug: temozolomide University of California, San Francisco Phase 2 1999-05-01 2015-05-28
    NCT00515788 Neoplastic Meningitis Drug: DepoCyt|Drug: Temozolomide M.D. Anderson Cancer Center|Enzon Pharmaceuticals, Inc.|Schering-Plough Phase 1 2006-02-01 2012-03-08
    NCT01205828 Hepatocellular Carcinoma Drug: Temozolomide|Drug: ABT-888 Georgetown University|Abbott Phase 2 2010-08-01 2017-01-17
    NCT00614978 Metastatic Breast Cancer|Brain Metastases|HER2 Positive Drug: lapatinib and temozolomide Jules Bordet Institute|GlaxoSmithKline|Schering-Plough Phase 1 2008-01-01 2012-09-18
    NCT01127594 Melanoma Drug: Temozolomide Douglas Tyler|Merck Sharp & Dohme Corp.|Duke University|M.D. Anderson Cancer Center|H. Lee Moffitt Cancer Center and Research Institute Phase 1 2010-07-01 2015-03-06

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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